For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA):
wherein each symbol is as defined in the specification.
or a salt thereof or a prodrug thereof.
Aza-Claisen Rearrangements Initiated by Acid-Catalyzed Michael Addition
作者:Edwin Vedejs、Marc Gingras
DOI:10.1021/ja00081a019
日期:1994.1
to protic acid catalysis and affords 15, the product of Michael addition and aza-Claisen rearrangement. The sequence involves Michael addition of 4c or 19-21 to generate an intermediateN-alkenyl ammonium salt 14 that undergoes a charge-accelerated rearrangement to 15. Toluenesulfonic acid is a useful catalyst for the Mickael addition step. Benzoic acid is not effective because the intermediate 14 is
烯丙胺与乙炔二甲酸二甲酯的反应在质子酸催化下得到 15,这是迈克尔加成和氮杂-克莱森重排的产物。该序列涉及4c或19-21的迈克尔加成以生成中间体N-烯基铵盐14,其经历电荷加速重排为15。甲苯磺酸是用于麦克尔加成步骤的有用催化剂。苯甲酸无效,因为中间体 14 被苯甲酸反离子竞争性脱烷基。在一种情况下,中间体 N-链烯基铵离子 18 已被 1 H NMR 光谱检测到,并已观察到在 -20 o C 下发生氮杂-克莱森重排
Cyclic Amine Compound and Use Thereof for the Prophylaxis or Treatment of Hypertension
申请人:Kuroita Takanobu
公开号:US20100121048A1
公开(公告)日:2010-05-13
The present invention relates to a compound represented by the formula: (I) wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent (s); U, V and W are each independently C or N, provided that when any one of U, V and W is N, then the others should be C; Ra and Rb are each independently a cyclic group optionally having substituent(s), a C
1-10
alkyl group optionally having substituent(s), a C
2-10
alkenyl group optionally having substituent(s), or a C
2-10
alkynyl group optionally having substituent(s); X is a bond, or a spacer having 1 to 6 atoms in the main chain; Y is a spacer having 1 to 6 atoms in the main chain; Rc is a hydrocarbon group optionally containing heteroatom(s) as the constituting atom(s), which optionally has substituent(s); m and n are each independently 1 or 2; and ring B optionally further has substituent(s), or a salt thereof. The compound of the present invention has excellent renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.
Reaction product and its use as additive conferring water resistance on ink compositions and colouring compositions and on paper
申请人:ORIENT CHEMICAL INDUSTRIES, LTD.
公开号:EP0147667A1
公开(公告)日:1985-07-10
There is provided hereby a water-resistant additive comprising a reaction mixture of
(a) a vinyl compound soluble in water or in a water soluble organic solvent, with
(b) an active hydrogen-containing compound which contains more than two groups having an active hydrogen respectively, at least one group of which is an amino group or imino group, or an active hydrogen-containing compound which contains a halogen group and an amino or imino group,
optionally in the presence of a solvent.